scholarly journals Once Daily Sustained-Release Matrix Tablet of Naproxen: Formulation and In Vitro Evaluation

1970 ◽  
Vol 9 (1) ◽  
pp. 47-52 ◽  
Author(s):  
Muhammad Rashedul Islam ◽  
Ishtiaq Ahmed ◽  
Mohiuddin Abdul Quadir ◽  
Md Habibur Rahman
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
In Vitro Release ◽  
Matrix Tablets ◽  
Matrix Tablet ◽  
Once Daily ◽  
Weight Variation ◽  
Release Studies ◽  
The Matrix

The objective of the present study was to develop once-daily sustained-release matrix tablets of naproxen, one of the most potent non-steroidal anti-inflammatory agents used in the treatment of arthritic pain. The tablets were prepared by direct compression method using hydrophilic matrix materials like Methocel® K4M CR and Methocel® K15M CR. The tablets were subjected to measurement of thickness, diameter, weight variation, drug content, hardness and friability, the results of which were within compendial specification range. In vitro release studies were carried out by the USP basket method and were carried out at pH 7.4 buffer for ten hours. The results of dissolution studies indicated that higher polymer content in the matrix (40%) decreased the release rate of the drug as shown in formulation NMK4MF6 and NMK15MF6 (where lactose content is zero). The most successful formulations of the study, exhibited satisfactory drug release which was very close to the theoretical release profile. All the formulations exhibited diffusion-dominated drug release. Key words: Naproxen; Methocel® K4M CR; Methocel® K15M CR; Sustained release; Matrix tablets DOI: 10.3329/dujps.v9i1.7429 Dhaka Univ. J. Pharm. Sci. 9(1): 47-52 2010 (June)

scholarly journals In vitro Release Kinetics Study of Ranolazine from Swellable Hydrophilic Matrix Tablets

1970 ◽  
Vol 8 (1) ◽  
pp. 31-38 ◽  
Author(s):  
Mohammad Nezab Uddin ◽  
Ishtiaq Ahmed ◽  
Monzurul Amin Roni ◽  
Muhammad Rashedul Islam ◽  
Mohammad Habibur Rahman ◽  
...  
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Release Kinetics ◽  
In Vitro Release ◽  
High Viscosity ◽  
Matrix Tablets ◽  
Release Studies ◽  
The Matrix ◽  
Vitro Release

The objective of this study was to design oral sustained release matrix tablets of Ranolazine usinghydroxypropyl methylcellulose (HPMC) as the retardant polymer and to study the effect of formulation factors suchas polymer proportion and polymer viscosity on the release of drug. In vitro release studies were performed usingUSP type II apparatus (paddle method) in 900 mL of 0.1N HCl at 100 rpm for 12 hours. The release kinetics wasanalyzed using the zero-order, first order, Higuchi and Korsmeyer-Peppas equations to explore and explain themechanism of drug release from the matrix tablets. In vitro release studies revealed that the release rate decreasedwith increase in polymer proportion and viscosity grade. Mathematical analysis of the release kinetics indicated thatthe nature of drug release from the matrix tablets was dependent on drug diffusion and polymer relaxation andtherefore followed non-Fickian or anomalous release. The developed controlled release matrix tablets of Ranolazineprepared with high viscosity HPMC extended release up to 12 hours.Key words: Ranolazine; Sustained release; Methocel E50 Premium LV; Methocel K100LV CR; Methocel K4M CR;Methocel K15M CR.DOI: 10.3329/dujps.v8i1.5333Dhaka Univ. J. Pharm. Sci. 8(1): 31-38, 2009 (June)

Effects of release modifier on Carvedilol release from Kollidon SR based matrix

2012 ◽  
Vol 1 (8) ◽  
pp. 186 ◽  
Author(s):  
Urmi Das ◽  
Mohammad Salim Hossain
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Microcrystalline Cellulose ◽  
Matrix Tablets ◽  
Dissolution Time ◽  
Release Mechanism ◽  
Matrix Tablet ◽  
Weight Variation ◽  
The Matrix ◽  
Tablet Formulations

<p>Sustained release Carvedilol matrix tablets constituting Kollidon SR were developed in this study in an attempt to investigate the effect of release modifiers on the release profile of Carvedilol from matrix. Three matrix tablet formulations were prepared by direct compression of Kollidon SR in combination with release modifier (HPMC and Microcrystalline Cellulose) and magnesium stearate. Tablets containing only Kollidon SR with the active ingredient demonstrated a rapid rate of drug release. Incorporation of HPMC in the matrix tablet prolonged the release of drug but incorporation of Microcrystalline Cellulose showed superimposable release pattern with an initial burst effect as confirmed by mean dissolution time and Higuchi release rate data. After 7 hours of dissolution, Carvedilol release from the matrix systems were 91.42%, 83.41%, from formulation F1 and F2 respectively. Formulation F3 exhibited 100 % release at 4 hours. All the tablet formulations showed acceptable pharmaco-technical properties and complied with the in-house specifications for tablet weight variation, friability, hardness, thickness, and diameter. Prepared tablets also showed sustained release property for carvedilol. The drug release mechanism from the matrix tablets of F1 and F2 was found to be followed by Fickian and F3 by Non-Fickian mechanism.</p><p>DOI: <a href="http://dx.doi.org/10.3329/icpj.v1i8.11095">http://dx.doi.org/10.3329/icpj.v1i8.11095</a></p> <p>International Current Pharmaceutical Journal 2012, 1(8): 186-192</p>

scholarly journals Formulation and evaluation of bi-layer floating tablets of ziprasidone HCl and trihexyphenidyl HCl

2011 ◽  
Vol 47 (3) ◽  
pp. 545-553 ◽  
Author(s):  
Sathis Kumar Dinakaran ◽  
Santhos Kumar ◽  
David Banji ◽  
Harani Avasarala ◽  
Venkateshwar Rao
Keyword(s):  
Sustained Release ◽  
In Vitro Release ◽  
Chemical Properties ◽  
Matrix Tablets ◽  
In Vitro Dissolution ◽  
Floating Tablets ◽  
Ir Studies ◽  
Weight Variation ◽  
The Matrix

The purpose of this research study was to establish ziprasidone HCl NR 40 mg and trihexyphenidyl HCl SR 4mg in the form of bi-layer sustained release floating tablets. The tablets were prepared using sodium HPMC K4M / HPMC K15M as bio-adhesive polymers and sodium bicarbonate acting as a floating layer. Tablets were evaluated based on different parameters such as thickness, hardness, friability, weight variation, in vitro dissolution studies, content of active ingredient and IR studies. The physico-chemical properties of the finished product complied with the specifications. In vitro release from the formulation was studied as per the USP XXIII dissolution procedure. The formulations gave a normal release effect followed by sustained release for 12 h which indicates bimodal release of ziprasidone HCl from the matrix tablets. The data obtained was fitted to Peppas models. Analysis of n values of the Korsmeyer equation indicated that the drug release involved non-diffusional mechanisms. By the present study, it can be concluded that bi-layer tablets of ziprasidone HCl and trihexyphenidyl HCl will be a useful strategy for extending the metabolism and improving the bioavailability of Ziprasidone HCl and Trihexyphenidyl HCl.

scholarly journals Formulation and Evaluation of Gabapentin Sustained Release Matrix Tablet Using Hibiscus rosa sinensis Leaves Mucilage as Release Retardant

2021 ◽  
pp. 564-572
Author(s):  
P. Amsa ◽  
G. K. Mathan ◽  
S. Magibalan ◽  
E. K. Velliyangiri ◽  
T. Kalaivani ◽  
...  
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Magnesium Stearate ◽  
Matrix Tablets ◽  
Wet Granulation ◽  
Matrix Tablet ◽  
Hibiscus Rosa Sinensis

The major goal of this study was to develop and evaluate Sustained release matrix tablets of Gabapentin with Hibiscus rosa - sinensis leaves mucilage prepared by using wet granulation technique with microcrystalline cellulose as a diluents and magnesium stearate as a lubricant. Pre-compression and post-compression evaluation of physicochemical parameters were carried out and to be within acceptable limits. Drug and polymer compatibility were validated by FTIR measurements. Further, tablets were evaluated for in vitro release study. To get the sustained release of Gabapentin, the concentration of Hibiscus rosa- sinensis mucilage was tuned with a gas-generating agent. The % drug release of all formulation from F1 to F5 showed 91.24%, 80.24%, 70.53%, 62.12% and 49.83% respectively. All the dosage form release kinetics was computed using zero order, first order, Higuchi, and Korsmeyer–Peppas methods. From the above results, it is concluded that the n value of formulation F5 showed 0.78 suggesting anomalous (non-fickian) behavior of the drug. Mucilage from the leaves of Hibiscus rosa-sinensis has a great retarding effect in drug release from sustained release tablets.

scholarly journals FORMULATION AND EVALUATION OF COLON TARGETED MATRIX TABLET USING NATURAL TREE GUMS

2018 ◽  
Vol 10 (9) ◽  
pp. 92
Author(s):  
Poreddy Srikanth Reddy ◽  
Penjuri Subhash Chandra Bose ◽  
Damineni Saritha ◽  
Vuppula Sruthi
Keyword(s):  
Drug Release ◽  
In Vitro Release ◽  
Wet Granulation ◽  
Average Weight ◽  
Matrix Tablet ◽  
Weight Variation ◽  
Release Studies ◽  
Percentage Weight ◽  
Diltiazem Hcl

Objective: To develop a novel colon targeted tablet formulation using natural polysaccharides such as kondagogu gum and ghatti gum as carriers and diltiazem hydrochloride as a model drug.Methods: The polymer-drug tablets were prepared by wet granulation technique, coated with two layers viz., inulin as an inner coat followed by shellac as outer coat and evaluated for properties such as average weight, hardness and coat thickness. In vitro release studies of prepared tablets were carried out for 2 h in pH 1.2 HCl buffer, 3 h in pH 7.4 phosphate buffer and 6 h in simulated colonic fluid (SCF) in order to mimic the conditions from mouth to colon.Results: Percentage weight variation, percent friability and content of active ingredient for all the formulations were found to be well within United States Pharmacopoeia (USP) limits. Out of both the polymers, the tablets prepared with ghatti gum showed the maximum hardness of 7.1 kg/cm2. The FTIR spectra of pure diltiazem HCl and the formulation KF3 were found to be identical. From the DSC, it was evident that the melting point peak of diltiazem HCl and formulation KF3 were observed at 217.16 and 218.34 °C respectively. In vitro studies revealed that the tablets coated with shellac (2.5% w/w), prevented the drug release in stomach environment and inulin coated tablets (4% w/w) have limited the drug release in the small intestinal environment. The data obtained from in vitro drug release studies were fit into Peppas model and in all the cases the value of A was found to be more than 2, i.e., drug release by a combination of both diffusion and erosion-controlled drug release.Conclusion: The study revealed that polysaccharides as carriers and inulin and shellac as a coating material can be used effectively for colon targeting of drugs for treating local as well as systemic disorders.

scholarly journals Development and in-vitro Evaluation of Once Daily Tablet Dosage Form of Loxoprofen Sodium

2015 ◽  
Vol 14 (9) ◽  
pp. 1557-1563
Author(s):  
M Zaman ◽  
RM Sarfraz ◽  
S Adnan ◽  
A Mahmood ◽  
M Hanif ◽  
...  
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Matrix Tablets ◽  
Angle Of Repose ◽  
Fickian Diffusion ◽  
Once Daily ◽  
Drug Content ◽  
Weight Variation ◽  
Loxoprofen Sodium

Purpose: To formulate and characterize once daily controlled release tablet of loxoprofen sodium.Methods: Eudragit RS-100, hydroxylpropyl methylcellulose (HPMC) and pectin were used as release retarding polymers. All the formulations were prepared by direct compression method. Various precompression studies were carried out to determine Hausner’s ratio, Carr’s index, angle of repose, bulk density and tapped density Differential scanning calorimetry (DSC) studies and also post-compression studies to evaluate hardness, friability, weight variation, drug content, in-vitro drug release were conducted on the tablets. The drug release data were subjected to kinetic models, including zero order, first order, Hixon Crowell, Higuchi and Korsmeyer-Peppas.Results: Compressibility index (7.6 ± 1.32 - 12.5 ± 1.43%), Hausner’s ratio (1.08 ± 0.04 - 1.14 ± 0.03), angle of repose (27.78 ± 0.47 - 30.49 ± 0.46°), hardness (6.25 ± 0.27 - 7.21±0.21 kg/cm2), friability (0.14 ± 0.06 - 0.28 ± 0.0 %), weight variation (249.5 ± 2.09 - 251.35 ± 2.41 mg) and drug content  (97.30 ± 0.28 - 103.70 ± 0.31 %) were within generally accepted limits for the pre-and post-compression formulations, respectively. The tablets having the maximum amount of among the three polymers tested as matrix materials, HPMC, represented by F3 tablets, exerted better sustained release properties after 12 h. Release pattern was more of Fickian diffusion followed by Higuchi mechanism.Conclusion: The release of the loxoprofen sodium was optimized up to 12 h.Keywords: Loxoprofen, Sustained release, hydroxypropyl methylcelluose, Pectin, Eudragit, Matrix tablets

scholarly journals Formulation and Development Matrix Tablets Of Methimazole

2021 ◽  
Vol 11 (5) ◽  
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Half Life ◽  
In Vitro Release ◽  
Methyl Cellulose ◽  
Clinical Effectiveness ◽  
Active Pharmaceutical Ingredient ◽  
Matrix Tablets ◽  
Matrix Tablet

Methimazole is active pharmaceutical ingredient effectively utilized in hyperthyroidism. Methimazole inhibits peroxidase as well as iodine interactions with thyroglobulin to produce triiodothyronine with thyroxine. Methimazole shows very low protein binding (1-10%) bounds to plasma proteins and easily metabolized by liver. In this investigation, efforts given to develop a sustained release matrix tablet of Methimazole. Sustained release drug delivery systems are for a maximum of 24 hours clinical effectiveness. Such systems are primarily for the drugs of short elimination half-life. However, drugs with long half-life also qualify if a reduction in steady state fluctuation is desired. Matrix tablets of methimazole were prepared by utilizing direct compression method. HPMC along with Sodium carboxy methyl cellulose used to retard drug release from the dosage form. Matrix tablets of methimazole were evaluated for different quality control test to improve quality of the product. In vitro release study of methimazole matrix tablets shows that polymer percentage used in the formula is enough to extend the release of the drug for at least 12 hr. In dissolution study of matrix of methimazole formulation F2 shows maximum drug release 97.93 % at the end of 6 hours while F1 shows least 83.64 %. Keywords: Matrix tablet, Methimazole, Sustained Release

scholarly journals Effects of release modifier on Carvedilol release from Kollidon SR based matrix

2012 ◽  
Vol 1 (8) ◽  
pp. 186-192 ◽  
Author(s):  
Urmi Das ◽  
Mohammad Salim Hossain
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Microcrystalline Cellulose ◽  
Matrix Tablets ◽  
Dissolution Time ◽  
Release Mechanism ◽  
Matrix Tablet ◽  
Weight Variation ◽  
The Matrix ◽  
Tablet Formulations

Sustained release Carvedilol matrix tablets constituting Kollidon SR were developed in this study in an attempt to investigate the effect of release modifiers on the release profile of Carvedilol from matrix. Three matrix tablet formulations were prepared by direct compression of Kollidon SR in combination with release modifier (HPMC and Microcrystalline Cellulose) and magnesium stearate. Tablets containing only Kollidon SR with the active ingredient demonstrated a rapid rate of drug release. Incorporation of HPMC in the matrix tablet prolonged the release of drug but incorporation of Microcrystalline Cellulose showed superimposable release pattern with an initial burst effect as confirmed by mean dissolution time and Higuchi release rate data. After 7 hours of dissolution, Carvedilol release from the matrix systems were 91.42%, 83.41%, from formulation F1 and F2 respectively. Formulation F3 exhibited 100 % release at 4 hours. All the tablet formulations showed acceptable pharmaco-technical properties and complied with the in-house specifications for tablet weight variation, friability, hardness, thickness, and diameter. Prepared tablets also showed sustained release property for carvedilol. The drug release mechanism from the matrix tablets of F1 and F2 was found to be followed by Fickian and F3 by Non-Fickian mechanism.DOI: http://dx.doi.org/10.3329/icpj.v1i8.11248 International Current Pharmaceutical Journal 2012, 1(8): 186-192 

scholarly journals Release Profile of Losartan Potassium from Formulated Sustained Release Matrix Tablet

2015 ◽  
Vol 16 (2) ◽  
pp. 177-183
Author(s):  
Md Ziaur Rahman ◽  
Sayed Koushik Ahamed ◽  
Sujan Banik ◽  
Mohammad Salim Hossain
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Methyl Cellulose ◽  
Matrix Tablets ◽  
Losartan Potassium ◽  
Matrix Tablet ◽  
Vitro Release

The present study was undertaken to develop sustained release (SR) matrix tablets of Losartan potassium, an angiotensin-II antagonist for the treatment of hypertension. The tablets were prepared by direct compression method along with Kollidon SR and Methyl Cellulose as release retardant polymers. The evaluation involves two stages- the physical properties studies of tablets and in vitro release kinetics assessment. The USP paddle method was selected to perform the dissolution test and 900 ml phosphate buffer of pH 6.8 was used as dissolution medium at 50 rpm at 370C. The release kinetics were analyzed. All the formulations followed Higuchi release kinetics. When the release data was plotted into Korsmeyer-Peppas equation, then it was confirmed that F-1, F-2, F-3, F-4 and F-5 exhibited non-fickian type drug release whereas F-6 exhibited fickian type drug release from the tablet matrix. The in-vitro release studies revealed that the formulation F-2 can be taken as an ideal or optimized formulation of sustained release tablets for 24 hours release as it fulfills all the requirements for sustained release tablet. Furthermore, when the tablets were preheated at different temperature (300C, 450C, 600C) before dissolution they showed decrease in drug release compared with ambient temperature DOI: http://dx.doi.org/10.3329/bpj.v16i2.22301 Bangladesh Pharmaceutical Journal 16(2): 177-183, 2013

Formulation and Evaluation of Galantamine Hydrobromide Floating Matrix Tablet

2018 ◽  
Vol 8 (2) ◽  
Author(s):  
Poreddy Srikanth Reddy ◽  
Penjuri Subhash Chandra Bose ◽  
Vuppula Sruthi ◽  
Damineni Saritha
Keyword(s):  
Sodium Alginate ◽  
Xanthan Gum ◽  
Lag Time ◽  
Matrix Tablets ◽  
In Vitro Dissolution ◽  
Matrix Tablet ◽  
Compression Technique ◽  
Weight Variation ◽  
The Matrix

The aim of the present work was to prepare floating tablets of galantamine HBr using sodium alginate and xanthan gum as matrix forming carriers. Galantamine HBr is used for the treatment of mild to moderate Alzheimer's disease and various other memory impairments, in particular those of vascular origin. The matrix tablet formulations were prepared by varying the concentrations of sodium alginate and xanthan gum. The tablets were prepared by direct compression technique using PVP K-30 as a binder and sodium bicarbonate for development of CO2. The prepared matrix tablets were evaluated for properties such as hardness, thickness, friability, weight variation, floating lag time, compatibility using DSC and FTIR. In vitro dissolution was carried out for 12 hrs in 0.1N HCl at 37±0.5 ºC using USP paddle type dissolution apparatus. It was noted that, all the prepared formulations had desired floating lag time and constantly floated on dissolution medium by maintaining the matrix integrity. The drug release from prepared tablets was found to vary with varying concentration of the polymers, sodium alginate and xanthan gum. From the study it was concluded that floating drug delivery system for galantamine HBr can be prepared by using sodium alginate and xanthan gum as a carrier.

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